On November 29, 2018, Li, Liansheng; Feng, Jun; Wu, Tao; Liu, Yuan; Wang, Yi; Ren, Pingda; Liu, Yi published a patent.SDS of cas: 1620510-51-1 The title of the patent was Preparation of substituted quinazolines as covalent inhibitors of KRAS. And the patent contained the following:
The title compounds I [G1 and G2 = (independently) N or CH; L1 = a bond or NR6; L2 = a bond or alkylene; L3 = a bond, O, NR6, S, S(O) or SO2; R1 = unsubstituted naphthyl or optionally substituted quinolinyl when at least one of R31, R32, R41 and R42 is not H; or R1 = II (A1-A4 = (independently) C or N; X = O, S, N, etc.;Y = O, S, N, etc.; Z = O, S, N, etc.; one of R11-R14 is a covalent bond to the carbon attached to R1, and the other of R11-R14 = (independently) H, NH2, CN, etc.; R21-R23 = (independently) H, NH2, CN, etc.; R31 and R32 = (independently) H, OH, NH2, etc.; R41 and R42 = (independently) H, OH, NH2, etc.; R5 = NH2, CN, OH, etc.; R6 = (independently) H or alkyl; m and n = (independently) 1-3; and E = an electrophilic moiety capable of forming a covalent bond with the cysteine residue at position 12 of a KRAS, HRAS or NRAS G12C mutant protein)] or pharmaceutically acceptable salts, isotopic forms, stereoisomers or prodrugs thereof, having activity as inhibitors of G12C mutant KRAS protein, were prepared E.g., a multi-step synthesis of (2R,5S)-III, starting from 2-amino-4-bromo-3-fluorobenzoic acid, was described. Representative compounds I were tested and found to covalently bind to (or modify) KRAS G12C after a ten minute incubation period (data given). Pharmaceutical compositions comprising compounds I, and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, were also provided. The experimental process involved the reaction of (R)-(4-Methylmorpholin-3-yl)methanol(cas: 1620510-51-1).SDS of cas: 1620510-51-1
The Article related to quinazoline preparation g12c mutant kras inhibitor antitumor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.SDS of cas: 1620510-51-1
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